Ticagrelor - ≥98%, high purity , Purinergic receptor P2Y12 negative allosteric modulator, CAS No.274693-27-5, Purinergic receptor P2Y12 negative allosteric modulator

Item Number
T125095
Grouped product items
SKUSizeAvailabilityPrice Qty
T125095-25mg
25mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$9.90
T125095-250mg
250mg
In stock
$9.90
T125095-500mg
500mg
In stock
$13.90
T125095-1g
1g
In stock
$18.90
T125095-5g
5g
In stock
$65.90

Reversible P2Y 12 receptor antagonist

Basic Description

SynonymsTICAGRELOR [ORANGE BOOK] | TICAGRELOR [USP-RS] | SCHEMBL1979652 | (1s,2s,3r,5s)-3-[7-[[(1r,2s)-2-(3,4-difluorophenyl)-cyclopropyl]amino]-5-(propylthio)-3h-[1,2,3]-triazolo[4,5-d]pyrimidine-3-yl]-5-(2-hydroxyethoxy) cyclopentane-1,2-diol | (1S,2S,3R,5S)-3-
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsTicagrelor is an active drug which, does not require metabolic activation after intestinal absorption. It does not compete directly with ADP at the ADP binding site but occupies an adjacent binding site and acts in an allosteric way, resulting in a revers
Storage TempProtected from light,Store at -20°C,Argon charged
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeANTAGONIST, INHIBITOR, NEGATIVE ALLOSTERIC MODULATOR
Mechanism of actionPurinergic receptor P2Y12 negative allosteric modulator
Product Description

Ticagrelor(AZD-6140) is the first reversibly binding oral P2Y12 receptor antagonist(Ki= 2 nM), also inhibits CYP2C9 and midazolam 4-hydroxylation with IC50 of 10.5 μM and 8.2 μM respectively.
A reversible antagonist of the platelet purinergic P2Y12 receptor

Product Properties

ALogP2

Associated Targets(Human)

SLC29A1 Tclin Equilibrative nucleoside transporter 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
P2RY12 Tclin P2Y purinoceptor 12 (6 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
F2 Tclin Thrombin (11687 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ESR1 Tclin Estrogen receptor alpha (17718 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PGR Tclin Progesterone receptor (8562 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AR Tclin Androgen Receptor (11781 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GABRA1 Tclin GABA receptor alpha-1 subunit (399 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ACHE Tclin Acetylcholinesterase (18204 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTGS1 Tclin Cyclooxygenase-1 (9233 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
XDH Tclin Xanthine dehydrogenase (1038 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PDE3A Tclin Phosphodiesterase 3A (3309 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC29A1 Tclin Equilibrative nucleoside transporter 1 (1711 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
P2RY12 Tclin Purinergic receptor P2Y12 (2369 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TBXA2R Tclin Thromboxane A2 receptor (5717 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PDE4A Tclin Phosphodiesterase 4A (1943 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA3 Tchem Adenosine A3 receptor (15931 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HRH3 Tclin Histamine H3 receptor (10389 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KDR Tclin Vascular endothelial growth factor receptor 2 (20924 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
S1PR1 Tclin Sphingosine 1-phosphate receptor Edg-1 (5806 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GLP1R Tclin Glucagon-like peptide 1 receptor (111429 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
C5AR1 Tclin C5a anaphylatoxin chemotactic receptor (2677 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Homo sapiens (32628 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CX3CR1 Tchem C-X3-C chemokine receptor 1 (1686 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
FPR2 Tchem Lipoxin A4 receptor (3472 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
FFAR4 Tchem G-protein coupled receptor 120 (2999 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GPR35 Tchem G-protein coupled receptor 35 (2643 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A (122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Aplnr Apelin receptor (201 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mapk1 MAP kinase ERK2 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Staphylococcus aureus (210822 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Canis familiaris (36305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Gpr119 Glucose-dependent insulinotropic receptor (270 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Plasma (328 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver microsome (341 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name (1S,2S,3R,5S)-3-[7-[[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino]-5-propylsulfanyltriazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol
INCHI InChI=1S/C23H28F2N6O4S/c1-2-7-36-23-27-21(26-15-9-12(15)11-3-4-13(24)14(25)8-11)18-22(28-23)31(30-29-18)16-10-17(35-6-5-32)20(34)19(16)33/h3-4,8,12,15-17,19-20,32-34H,2,5-7,9-10H2,1H3,(H,26,27,28)/t12-,15+,16+,17-,19-,20+/m0/s1
InChi Key OEKWJQXRCDYSHL-FNOIDJSQSA-N
Canonical SMILES CCCSC1=NC(=C2C(=N1)N(N=N2)C3CC(C(C3O)O)OCCO)NC4CC4C5=CC(=C(C=C5)F)F
Isomeric SMILES CCCSC1=NC(=C2C(=N1)N(N=N2)[C@@H]3C[C@@H]([C@H]([C@H]3O)O)OCCO)N[C@@H]4C[C@H]4C5=CC(=C(C=C5)F)F
PubChem CID 9871419
Molecular Weight 522.57

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

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15 results found

Lot NumberCertificate TypeDateItem
A2306899Certificate of AnalysisOct 22, 2024 T125095
A2306882Certificate of AnalysisOct 22, 2024 T125095
A2306865Certificate of AnalysisOct 22, 2024 T125095
A2306734Certificate of AnalysisOct 22, 2024 T125095
A2306735Certificate of AnalysisOct 11, 2024 T125095
A2306881Certificate of AnalysisOct 11, 2024 T125095
A2306883Certificate of AnalysisOct 11, 2024 T125095
H2229660Certificate of AnalysisJun 20, 2024 T125095
K2323489Certificate of AnalysisNov 11, 2023 T125095
K2323490Certificate of AnalysisNov 11, 2023 T125095
I2116363Certificate of AnalysisJul 07, 2023 T125095
I2116390Certificate of AnalysisJul 07, 2023 T125095
A2306863Certificate of AnalysisSep 22, 2022 T125095
L1613016Certificate of AnalysisJul 19, 2022 T125095
K1826070Certificate of AnalysisJul 13, 2022 T125095

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Chemical and Physical Properties

SolubilityDMSO 105 mg/mL Water <1 mg/mL Ethanol 53 mg/mL
SensitivityLight sensitive
Refractive Index1.74
Boil Point(°C)~777.6 °C at 760 mmHg
Melt Point(°C)149-154°C

Safety and Hazards(GHS)

Pictogram(s) GHS09,   GHS07
Signal Warning
Hazard Statements

H315:Causes skin irritation

H319:Causes serious eye irritation

H335:May cause respiratory irritation

H411:Toxic to aquatic life with long lasting effects

Precautionary Statements

P261:Avoid breathing dust/fume/gas/mist/vapors/spray.

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

P273:Avoid release to the environment.

P280:Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352:IF ON SKIN: wash with plenty of water.

P321:Specific treatment (see ... on this label).

P405:Store locked up.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P271:Use only outdoors or in a well-ventilated area.

P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing.

P403+P233:Store in a well-ventilated place. Keep container tightly closed.

P362+P364:Take off contaminated clothing and wash it before reuse.

P391:Collect spillage.

P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes.

P337+P317:If eye irritation persists: Get medical help.

P332+P317:If skin irritation occurs: Get medical help.

P319:Get medical help if you feel unwell.

Related Documents

Citations of This Product

1. Zhang Shengshuo, Cheng Yueqing, Gao Yujie, Zou Yujie, Xiao Weiling, Li Tianyi, Li Mei, Yu Bowen, Dong Jinhua.  (2023)  Fluorescence quenching-based immunological probe for ticagrelor monitoring.  Frontiers in Bioengineering and Biotechnology,  11    [PMID:38090713] [10.3389/fbioe.2023.1295406]
2. Xue Ying, Wang Ziteng, Cai Weimin, Tian Xin, Liu Shuaibing.  (2021)  A Validated LC–MS/MS Method for the Simultaneous Determination of Ticagrelor, Its Two Metabolites and Major Constituents of Tea Polyphenols in Rat Plasma and Its Application in a Pharmacokinetic Study.  JOURNAL OF CHROMATOGRAPHIC SCIENCE,  59  (6): (510-520).  [PMID:33634314] [10.1093/chromsci/bmab012]
3. Jia Chong, Hao Chen, Dapeng Dai, Shuanghu Wang, Quan Zhou, Junpeng Liu, You Lü, Hualan Wu, Minghui Du, Feifei Chen, Hui Jiang, Yunfang Zhou, Jiefu Yang.  (2020)  Effects of ticagrelor on the pharmacokinetics of rivaroxaban in rats.  PHARMACEUTICAL BIOLOGY,      [PMID:32633174] [10.1080/13880209.2020.1785510]
4. Xiaoyu Wang, Xuejie Han, Minghui Li, Yu Han, Yun Zhang, Shiqi Zhao, Yue Li.  (2018)  Ticagrelor protects against AngII-induced endothelial dysfunction by alleviating endoplasmic reticulum stress.  MICROVASCULAR RESEARCH,  119  (98).  [PMID:29777791] [10.1016/j.mvr.2018.05.006]

References

1. Springthorpe B, Bailey A, Barton P, Birkinshaw TN, Bonnert RV, Brown RC, Chapman D, Dixon J, Guile SD, Humphries RG et al..  (2007)  From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis..  Bioorg Med Chem Lett,  17  (21): (6013-8).  [PMID:17827008] [10.1021/op500134e]
2. Zhang Shengshuo, Cheng Yueqing, Gao Yujie, Zou Yujie, Xiao Weiling, Li Tianyi, Li Mei, Yu Bowen, Dong Jinhua.  (2023)  Fluorescence quenching-based immunological probe for ticagrelor monitoring.  Frontiers in Bioengineering and Biotechnology,  11    [PMID:38090713] [10.3389/fbioe.2023.1295406]
3. Xue Ying, Wang Ziteng, Cai Weimin, Tian Xin, Liu Shuaibing.  (2021)  A Validated LC–MS/MS Method for the Simultaneous Determination of Ticagrelor, Its Two Metabolites and Major Constituents of Tea Polyphenols in Rat Plasma and Its Application in a Pharmacokinetic Study.  JOURNAL OF CHROMATOGRAPHIC SCIENCE,  59  (6): (510-520).  [PMID:33634314] [10.1093/chromsci/bmab012]
4. Jia Chong, Hao Chen, Dapeng Dai, Shuanghu Wang, Quan Zhou, Junpeng Liu, You Lü, Hualan Wu, Minghui Du, Feifei Chen, Hui Jiang, Yunfang Zhou, Jiefu Yang.  (2020)  Effects of ticagrelor on the pharmacokinetics of rivaroxaban in rats.  PHARMACEUTICAL BIOLOGY,      [PMID:32633174] [10.1080/13880209.2020.1785510]
5. Xiaoyu Wang, Xuejie Han, Minghui Li, Yu Han, Yun Zhang, Shiqi Zhao, Yue Li.  (2018)  Ticagrelor protects against AngII-induced endothelial dysfunction by alleviating endoplasmic reticulum stress.  MICROVASCULAR RESEARCH,  119  (98).  [PMID:29777791] [10.1016/j.mvr.2018.05.006]

Solution Calculators